WordNet

make a score (on a hole) equal to par
(golf) the standard number of strokes set for each hole on a golf course, or for the entire course; "a par-5 hole"; "par for this course is 72"
the 16th letter of the Roman alphabet (同)p

PrepTutorEJDIC

〈U〉同等,同価,同水準,同程度 / (また『par value』)〈U〉平価,額面価格 / 〈U〉(程度・質・状態・数量などの)平均,標準;(精神・健康などの)常態 / 〈C〉(ゴルフで)標準打数,パー / 《名詞の前にのみ用いて》平均の,標準の / 額面の
(ゴルフで)〈1ホールまたは1コース〉‘を'基準打数でとる,パーで上がる
personal assistant個人秘書 / public address [system]
parking
phosphorusの化学記号

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/09/29 01:48:32」(JST)

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Protease activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is a protein that in humans is encoded by the F2RL1 gene. PAR2 modulates inflammatory responses and acts as a sensor for proteolytic enzymes generated during infection.^[1]

Gene

The F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence.^[2]

Mechanism of activation

PAR2 is a member of the large family of 7-transmembrane receptors that couple to guanosine-nucleotide-binding proteins. PAR2 is also a member of the protease-activated receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. Additionally, these receptors can be activated by exogenous proteases, such as house dust mite protein Der P9.^[3] These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand.^[4]

Agonists and antagonists

Potent and selective small molecule agonists and antagonists for PAR2 have been discovered.^[5]^[6]

References

^ Lee SE, Jeong SK, Lee SH (November 2010). "Protease and protease-activated receptor-2 signaling in the pathogenesis of atopic dermatitis". Yonsei Med. J. 51 (6): 808–22. doi:10.3349/ymj.2010.51.6.808. PMC 2995962. PMID 20879045.
^ "Entrez Gene: F2RL1 coagulation factor II (thrombin) receptor-like 1".
^ Sun G, Stacey MA, Schmidt M, Mori L, Mattoli S (July 2001). "Interaction of mite allergens Der p3 and Der p9 with protease-activated receptor-2 expressed by lung epithelial cells". J. Immunol. 167 (2): 1014–21. doi:10.4049/jimmunol.167.2.1014. PMID 11441110.
^ Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M, Sekiguchi F, Kubo S, Kuroda R, Iwaki M, Katsura K, Plevin R (June 2004). "Potent and metabolically stable agonists for protease-activated receptor-2: evaluation of activity in multiple assay systems in vitro and in vivo". J. Pharmacol. Exp. Ther. 309 (3): 1098–107. doi:10.1124/jpet.103.061010. PMID 14976227.
^ Gardell LR, Ma JN, Seitzberg JG, Knapp AE, Schiffer HH, Tabatabaei A, Davis CN, Owens M, Clemons B, Wong KK, Lund B, Nash NR, Gao Y, Lameh J, Schmelzer K, Olsson R, Burstein ES (December 2008). "Identification and characterization of novel small-molecule protease-activated receptor 2 agonists". J. Pharmacol. Exp. Ther. 327 (3): 799–808. doi:10.1124/jpet.108.142570. PMID 18768780.
^ Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP (October 2010). "Novel agonists and antagonists for human protease activated receptor 2". J. Med. Chem. 53 (20): 7428–40. doi:10.1021/jm100984y. PMID 20873792.

External links

"Protease-Activated Receptors: PAR2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

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English Journal

Glycyrrhetinic acid prevents cutaneous scratching behavior in mice elicited by substance P or PAR-2 agonist.

Akasaka Y, Yoshida T, Tsukahara M, Hatta A, Inoue H.AbstractAlthough glycyrrhetinic acid (GA) has been used for the prevention of itch in chronic dermatitis, the mechanism underlying the antipruritic effects of GA is still unclear. Recently, several mediators other than histamine, such as substance P and tryptase, were found to participate in chronic itch. Here, we investigated the effect of GA on pruritus induced by various pruritic agents including histamine in mice. We also determined the level of leukotriene (LT)B(4) in mouse skin injected with substance P in an effort to uncover part of the antipruritic mechanism of GA. Scratching events were counted for 10min after intradermal injection of histamine, substance P (100nmol per site each), protease-activated receptor-2 (PAR-2) agonistic peptide (50nmol per site), or LTB(4) (0.03nmol per site) with or without GA (4nmol per site) into male ICR mice. Levels of LTB(4) in the skin after injection of substance P were determined by ELISA. GA did not suppress scratching behavior induced by histamine and LTB(4), but markedly and dose-dependently suppressed that induced by substance P and PAR-2 agonistic peptide. LTB(4) levels in skin elevated by substance P were lowered by GA. These data support the efficacy of GA in counteracting itch in chronic dermatitis because GA reduced scratching behavior induced by substance P and PAR-2 agonistic peptide. GA may exert antipruritic effects via inhibition of LTB(4) production in skin.
European journal of pharmacology.Eur J Pharmacol.2011 Nov 16;670(1):175-9. Epub 2011 Sep 10.
Although glycyrrhetinic acid (GA) has been used for the prevention of itch in chronic dermatitis, the mechanism underlying the antipruritic effects of GA is still unclear. Recently, several mediators other than histamine, such as substance P and tryptase, were found to participate in chronic itch. H
PMID 21925497

Redox regulation of human protease-activated receptor-2 by activated factor X.

Jobi K, Rauch BH, Dangwal S, Freidel K, Doller A, Eberhardt W, Fischer JW, Schror K, Rosenkranz AC.SourceInstitut fur Pharmakologie und Klinische Pharmakologie, Heinrich-Heine-Universitat Dusseldorf, 40225 Dusseldorf, Germany.
Free radical biology & medicine.Free Radic Biol Med.2011 Nov 1;51(9):1758-64. Epub 2011 Aug 12.
Activated factor X (FXa) exerts coagulation-independent actions such as proliferation of vascular smooth muscle cells (SMCs) through the protease-activated receptors PAR-1 and PAR-2. Both receptors are upregulated upon vascular injury but the underlying mechanisms have not been defined. We examined
PMID 21871560

Japanese Journal

P2-10-20 子宮頸癌のリンパ節転移におけるprotease activated receptor (PAR)-2の発現の臨床的意義(Group85 子宮頸部腫瘍・基礎,一般演題,第63回日本産科婦人科学会学術講演会)

藤本次良,佐藤英理子,豊木廣,森重健一郎
日本産科婦人科學會雜誌 63(2), 749, 2011-02-01
NAID 110008509668

日本人幼児における日常の身体活動量と生活環境の関係

田中千晶,田中茂穂,安藤貴史
発育発達研究 2011(51), 51_37-51_45, 2011
… Presence of hills was significantly associated with less time in PAR (physical activity ratio)≥4. … On the other hand, relationships between the amount of time in 2>=PAR<3 and fatigue and between the amount of time in PAR<2 or 2>=PAR<3 and motion sickness were significant. …
NAID 130000954020

★リンクテーブル★

リンク元	「プロテアーゼ活性化受容体2」「protease-activated receptor 2」「proteinase-activated receptor 2」
拡張検索	「PAR-2 receptor」「PAR-2受容体」「PAR-2レセプター」
関連記事	「PA」「PAR」「P」「par」

「プロテアーゼ活性化受容体2」

Coagulation factor II (thrombin) receptor-like 1
Identifiers
Symbols	F2RL1 ; GPR11; PAR2
External IDs	OMIM: 600933 MGI: 101910 HomoloGene: 21087 IUPHAR: PAR2 ChEMBL: 5963 GeneCards: F2RL1 Gene
Gene ontology
Molecular function	• G-protein alpha-subunit binding; • receptor activity; • G-protein coupled receptor activity; • receptor binding; • protein binding; • thrombin receptor activity; • G-protein beta-subunit binding;
Cellular component	• Golgi apparatus; • plasma membrane; • integral component of plasma membrane; • pseudopodium;
Biological process	• T cell activation involved in immune response; • positive regulation of leukocyte chemotaxis; • positive regulation of cytokine secretion involved in immune response; • positive regulation of glomerular filtration; • inflammatory response; • G-protein coupled receptor signaling pathway; • positive regulation of cytosolic calcium ion concentration; • blood coagulation; • negative regulation of tumor necrosis factor-mediated signaling pathway; • positive regulation of phosphatidylinositol 3-kinase signaling; • regulation of blood coagulation; • positive regulation of cell migration; • positive regulation of actin filament depolymerization; • positive regulation of pseudopodium assembly; • positive regulation of superoxide anion generation; • positive regulation of toll-like receptor 2 signaling pathway; • negative regulation of toll-like receptor 3 signaling pathway; • positive regulation of toll-like receptor 3 signaling pathway; • positive regulation of toll-like receptor 4 signaling pathway; • positive regulation of Rho protein signal transduction; • chemokine (C-C motif) ligand 2 secretion; • neutrophil activation; • regulation of I-kappaB kinase/NF-kappaB signaling; • positive regulation of I-kappaB kinase/NF-kappaB signaling; • positive regulation of eosinophil degranulation; • innate immune response; • positive regulation of vasodilation; • positive regulation of transcription from RNA polymerase II promoter; • regulation of JNK cascade; • negative regulation of JNK cascade; • positive regulation of JNK cascade; • interleukin-1 beta secretion; • leukocyte migration; • positive regulation of chemotaxis; • positive regulation of positive chemotaxis; • defense response to virus; • positive regulation of phagocytosis, engulfment; • establishment of endothelial barrier; • positive regulation of ERK1 and ERK2 cascade; • thrombin receptor signaling pathway; • leukocyte proliferation; • positive regulation of neutrophil mediated killing of gram-negative bacterium; • interleukin-10 secretion; • interferon-gamma secretion; • chemokine secretion; • negative regulation of chemokine secretion; • mature dendritic cell differentiation; • positive regulation of renin secretion into blood stream; • positive regulation of interleukin-8 secretion; • positive regulation of interleukin-6 secretion;
	Sources: Amigo / QuickGO
RNA expression pattern
	More reference expression data
Orthologs
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